Therapeutic compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-10358437-B2
Application number	US-201715449706-A
Country	US
Kind code	B2
Filing date	Mar 3, 2017
Priority date	Sep 5, 2014
Publication date	Jul 23, 2019
Grant date	Jul 23, 2019

Abstract

The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof:

wherein R 1 , R 3 -R 6 , X, and each R e have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

First claim

We claim:

1. A compound of formula (I), or a salt thereof:

wherein:
R 1 is selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and carbocyclyl;
R 3 is selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and carbocyclyl;

and the group:

is selected from the group consisting of:

provided that when R 1 is methyl, R 3 is methyl, X is N(H), R 4 is H, R 6 is H and each Re is CH 3 ;
then R 5 is not phenyl; and
provided the compound is not:

or a salt thereof.

2. The compound of claim 1 wherein the group:

is selected from the group consisting of:

3. The compound or salt of claim 1 , which is selected from the group consisting of:

or a salt thereof.

4. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof
and a pharmaceutically acceptable adjuvant, carrier, or vehicle.

5. A method for treating ovarian cancer or renal cell carcinoma in an animal comprising administering to the animal a compound of claim 1 or a pharmaceutically acceptable salt thereof.

6. A method of treating ovarian cancer or renal cell carcinoma in an individual comprising administering to the individual (a) a compound of claim 1 or a pharmaceutically acceptable salt thereof, and (b) a cytotoxic agent.

7. The compound of claim 1 , wherein R 1 is methyl.

8. The compound of claim 1 , wherein R 3 is methyl.

9. A method of treating ovarian cancer or renal cell carcinoma in an animal comprising administering to the animal a compound of formula:

or a pharmaceutically acceptable salt thereof.

Assignees

• Genentech Inc
• Constellation Pharmaceuticals Inc

Inventors

• Albrecht Brian K
• Cote Alexandre
• Crawford Terry
• Duplessis Martin
• Good Andrew Charles
• Leblanc Yves
• Magnuson Steven
• Nasveschuk Christopher G
• Pastor Richard
• Romero F Anthony
• Taylor Alexander M

Classifications

• C07D403/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title

• C07D249/12

  Oxygen or sulfur atoms · CPC title

• C07D401/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D403/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D253/075

  Two hetero atoms, in positions 3 and 5 · CPC title